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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists
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Reverse Yeast Two-hybrid System to Identify Mammalian Nuclear Receptor Residues that Interact with Ligands and/or Antagonists

Published on: November 15, 2013

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Natural ligands of RXR receptors

Patricia García1, Paula Lorenzo1, Angel R de Lera1

  • 1Departamento de Química Orgánica, Facultade de Química, CINBIO and IBIV, Universidade de Vigo, Campus As Lagoas-Marcosende, Vigo, Spain.

Methods in Enzymology
|May 4, 2020
PubMed

Insights

Retinoid X receptors (RXRs) are crucial for gene transcription. This study reviews natural rexinoids that bind RXRs and details the synthesis of a potential new RXR ligand.

Area of Science:

  • Molecular Biology
  • Endocrinology
  • Medicinal Chemistry

Background:

  • Retinoid X receptors (RXRs) are nuclear receptors that form heterodimers with other nuclear receptor superfamily members.
  • RXR ligands, or rexinoids, modulate gene transcription through interactions with these heterodimers.
  • Understanding rexinoid interactions is key to deciphering gene regulation.

Purpose of the Study:

  • To comprehensively review known natural products that bind to RXRs.
  • To describe the discovery methods for these natural rexinoids, including high-throughput screening and serendipity.
  • To provide synthetic protocols for a specific putative natural RXR ligand.

Main Methods:

  • Literature review of natural products binding RXRs.
  • Description of discovery methodologies (HTS, serendipity).
  • Detailed protocols for the stereoselective synthesis of (R)-9-cis-13,14-dihydroretinoic acid.

Main Results:

  • A curated collection of natural rexinoids is presented.
  • Various discovery pathways for RXR ligands are highlighted.
  • Successful diastereoselective and enantioselective synthesis of a dihydroretinoic acid analog is achieved.

Conclusions:

  • Natural rexinoids represent a diverse class of compounds modulating RXR activity.
  • The synthesis of (R)-9-cis-13,14-dihydroretinoic acid provides a valuable tool for further RXR research.
  • Further investigation into natural rexinoids can uncover novel therapeutic agents.
Keywords:
AgonistsNatural ligandsRXRRXR heterodimersRexinoidsSynthesis

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